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41. 发明申请

WO2004098591A3 INHIBITORS OF GLUTAMINYL CYCLASE AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISEASES 审中-公开
标题翻译：谷氨酰胺环化酶的抑制剂及其在治疗神经病中的应用
公开(公告)号：WO2004098591A3
公开(公告)日：2005-03-31
申请号：PCT/EP2004004773
申请日：2004-05-05
申请人： PROBIODRUG AG , DEMUTH HANS-ULRICH , HEISER ULRICH , BUCHHOLZ MIRKO , NIESTROJ ANDRE J , SCHILLING STEPHAN
发明人： DEMUTH HANS-ULRICH , HEISER ULRICH , BUCHHOLZ MIRKO , NIESTROJ ANDRE J , SCHILLING STEPHAN
IPC分类号： A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61P25/14 , A61P25/28 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/22 , C07D207/24 , C07D231/04 , C07D231/06 , C07D233/02 , C07D233/06 , C07D233/28 , C07D233/42 , C07D233/54 , C07D233/61 , C07D249/04 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/04 , C07D263/04 , C07D263/06 , C07D277/04 , C07D277/06 , C07D295/185 , C07D403/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
CPC分类号： C07D207/08 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D207/10 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/22 , C07D207/24 , C07D231/04 , C07D231/06 , C07D233/02 , C07D233/06 , C07D233/28 , C07D233/42 , C07D233/54 , C07D249/04 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/04 , C07D263/04 , C07D263/06 , C07D277/04 , C07D277/06 , C07D295/185 , C07D403/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07F9/5726 , C07F9/597 , C07F9/65066 , C07F9/6561
摘要： The present invention relates to compounds that act as inhibitors of QC including those represented by the general formulae ( 1 to 9): and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleepwakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
摘要翻译：本发明涉及作为QC抑制剂的化合物，包括由通式（1至9）表示的化合物及其组合用于治疗神经元疾病，特别是阿尔茨海默氏病，唐氏综合征，帕金森病，柯达亨廷顿氏菌，致病性精神病条件，精神分裂症，食物摄入受损，睡眠障碍，能量代谢的稳态调节受损，自主神经功能受损，激素平衡受损，调节受损，体液，高血压，发烧，睡眠失调，厌食，焦虑相关障碍，包括癫痫发作，药物戒断和酒精中毒，神经变性疾病，包括认知功能障碍和痴呆。

42. 发明申请

WO2004024061A3 ARYL-LINK-ARYL SUBSTITUTED THIAZOLIDINE-DIONE AND OXAZOLIDINE-DIONE AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译：作为钠通道阻断剂的ARYL-LINK-ARYL取代噻唑烷二酮和氧杂环丁酮
公开(公告)号：WO2004024061A3
公开(公告)日：2004-06-10
申请号：PCT/US0312910
申请日：2003-04-25
申请人： MERCK & CO INC , KUO HOWARD C H , AYER MICHELLE B , CHAKRAVARTY PRASUN K , MEINKE PETER T , PARSONS WILLIAM H , TYAGARAJAN SRIRAM
发明人： KUO HOWARD C H , AYER MICHELLE B , CHAKRAVARTY PRASUN K , MEINKE PETER T , PARSONS WILLIAM H , TYAGARAJAN SRIRAM
IPC分类号： A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/44 , C07D277/20 , C07D277/34 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14 , A61K31/44 , A61K31/42 , A61K31/425 , C07D263/04 , C07D277/04 , C07D401/00
CPC分类号： A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/44 , C07D277/20 , C07D277/34 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14
摘要： Aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds and a pharmaceutically acceptable carrier; and a method of treatment of acute pain, chronic pain, visceral pain, inflammatory pain, or neuropathic pain, as well as irritable bowel syndrome, Crohns disease, epilepsy, partial and generalized tonic seizures, multiple sclerosis, bipolar depression, and tachy-arrhythmias by the administration of an effective amount of aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are described.
摘要翻译：芳基 - 链接 - 芳基噻唑烷二酮和芳基 - 芳基恶唑烷二酮化合物是钠通道阻断剂; 包括有效量的芳基 - 链烷基 - 噻唑烷二酮和芳基 - 芳基恶唑烷二酮化合物和药学上可接受的载体的药物组合物; 以及治疗急性疼痛，慢性疼痛，内脏痛，炎症性疼痛或神经性疼痛以及肠易激综合征，克罗恩病，癫痫，部分和全身性强直性癫痫发作，多发性硬化，双相抑郁和快速性心律失常的方法通过施用有效量的芳基链接 - 芳基噻唑烷二酮和芳基 - 链烯基 - 恶唑烷二酮化合物。

43. 发明申请

WO03106456A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO03106456A2
公开(公告)日：2003-12-24
申请号：PCT/HU0300041
申请日：2003-06-11
申请人： SANOFI SYNTHELABO , ARANYI PETER , BALAZS LASZLO , BATA IMRE , BATORI SANDOR , BORONKAY EVA , KAPUI ZOLTAN , SUSAN EDIT , SZABO TIBOR , T NAGY LAJOS , URBAN-SZABO KATALIN , VARGA MARTON
发明人： ARANYI PETER , BALAZS LASZLO , BATA IMRE , BATORI SANDOR , BORONKAY EVA , KAPUI ZOLTAN , SUSAN EDIT , SZABO TIBOR , T NAGY LAJOS , URBAN-SZABO KATALIN , VARGA MARTON
IPC分类号： A61K31/439 , A61K31/444 , A61K31/496 , A61K31/506 , A61P3/00 , A61P3/10 , A61P13/12 , A61P17/00 , A61P25/18 , A61P25/22 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/06 , C07D207/16 , C07D263/06 , C07D277/06 , C07D451/04 , C07D451/14 , A61K31/46 , C07D263/04
CPC分类号： C07D451/04 , C07D207/06 , C07D207/16 , C07D263/06 , C07D277/06 , C07D451/14
摘要： The present invention relates to the novel compounds of the general formula (I) possessing DPP-IV inhibitory activity. These compounds contain tropane building blocks.
摘要翻译：本发明涉及具有DPP-IV抑制活性的通式（I）的新型化合物。这些化合物含有托烷组合物。

44. 发明申请

WO02056827A3 SUBSTITUTED FELBAMATE DERIVED COMPOUNDS 审中-公开
标题翻译：取代的FELBAMATE衍生化合物
公开(公告)号：WO02056827A3
公开(公告)日：2002-11-07
申请号：PCT/US0147665
申请日：2001-10-23
申请人： UNIV VIRGINIA , MACDONALD TIMOTHY L
发明人： MACDONALD TIMOTHY L
IPC分类号： A61K31/27 , A61K31/381 , A61P9/10 , A61P25/00 , A61P25/02 , A61P25/08 , A61P27/06 , C07C271/12 , C07D213/30 , C07D233/54 , C07D239/26 , C07D241/12 , C07D263/24 , C07D263/32 , C07D277/24 , C07D333/16 , A61K31/38 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/505 , C07C205/00 , C07D213/02 , C07D239/02 , C07D241/02 , C07D263/04 , C07D263/30 , C07D277/20 , C07D333/02
CPC分类号： C07D213/30 , C07C271/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D263/24 , C07D263/32 , C07D277/24 , C07D333/16
摘要： The present invention relates to novel felbamate derivatives and their use to threat neurological diseases such as epilepsy and neuropathic pain, and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.
摘要翻译：本发明涉及新颖的麦芽糖衍生物及其用于威胁神经系统疾病如癫痫和神经性疼痛的用途，并且用于治疗由缺血事件引起的组织损伤。纤维蛋白衍生物被修饰以防止被认为是造成与费尔班曼治疗相关的毒性的代谢物的形成。

45. 发明申请

WO0178654A3 HALOGENTATED 2-AMINO-3, 4 HEPTENOIC ACID DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 审中-公开
标题翻译：用作氮氧化物合酶抑制剂的氢化2-氨基-3,4-脱硫酸衍生物
公开(公告)号：WO0178654A3
公开(公告)日：2002-08-01
申请号：PCT/US0112262
申请日：2001-04-13
申请人： PHARMACIA CORP , HANSEN DONALD W JR , PITZELE BARNETT S , WEBBER RONALD KEITH , TOTH MIHALY V , AWASTHI ALOK K , TRIVEDI MAHIMA , MANNING PAMELA T , SIKORSKI JAMES A
发明人： HANSEN DONALD W JR , PITZELE BARNETT S , WEBBER RONALD KEITH , TOTH MIHALY V , AWASTHI ALOK K , TRIVEDI MAHIMA , MANNING PAMELA T , SIKORSKI JAMES A
IPC分类号： A61P1/04 , A61K31/198 , A61P11/00 , A61P17/02 , A61P19/02 , A61P25/00 , A61P27/12 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P43/00 , C07C229/30 , C07C257/14 , C07D209/48 , C07D263/04 , C07D263/06 , C07D413/06 , A61K31/44 , A61K31/22 , C07C61/16 , C07C69/74 , C07C229/00 , C07C251/00 , C07C269/00 , C07C315/00 , C07C321/00 , C07D211/70 , A61K314/215
CPC分类号： C07D209/48 , C07C257/14 , C07D263/04 , C07D263/06 , C07D413/06
摘要： The present invention contains halogenated 2-amino-3, 4 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：本发明包含可用作一氧化氮合酶抑制剂的卤代2-氨基-3,4-庚烯酸衍生物。

46. 发明申请

WO02038532A1 OPTICALLY ACTIVE AMINE DERIVATIVE AND METHOD OF SYNTHESIS 审中-公开
标题翻译：光活性胺衍生物和合成方法
公开(公告)号：WO02038532A1
公开(公告)日：2002-05-16
申请号：PCT/JP2001/009830
申请日：2001-11-09
IPC分类号： C07C213/02 , C07C213/08 , C07C215/30 , C07C271/18 , C07D263/04 , C07D263/06 , C07C215/46 , C07C269/06 , C07C271/16 , C07M7/00
CPC分类号： C07D263/04 , C07B2200/07 , C07C213/02 , C07C213/08 , C07C271/18 , C07D263/06 , C07C215/30
摘要： A natural type alpha -amino acid which is easily available and inexpensive is converted to a compound represented by the formula (1), which is reacted with an organometallic reagent represented by the formula (2) to obtain an optically active 5-hydroxyoxazolidine derivative represented by the formula (3). The derivative (3) is treated with an acid to obtain an optically active amino ketone derivative represented by the formula (4), which is subjected to reduction, etc. to obtain an optically active amino alcohol derivative represented by the formula (5) or (6). General formula (2) General formula (1) General formula (3) General formula (4) General formula (5) or General formula (6) Thus, the optically active amino alcohol derivative represented by the formula (5) or (6) having a satisfactory optical purity, which is useful as an intermediate for medicines, agricultural chemicals, etc., can be stereoselectively produced stably at low cost from a natural type alpha -amino acid as an easily available, inexpensive starting material without causing racemization. Also provided are: the optically active 5-hydroxyoxazolidine derivative represented by the formula (3) and the amino ketone derivative represented by the formula (4), which are important intermediates for this production; and processes for producing these.
摘要翻译：易于获得和便宜的天然α-阿氨酸被转化为式（1）表示的化合物，其与式（2）表示的有机金属试剂反应得到表示为光学活性的5-羟基恶唑烷衍生物通过式（3）。用酸处理衍生物（3），得到式（4）表示的光学活性氨基酮衍生物，进行还原等，得到式（5）表示的光学活性氨基醇衍生物或式（6）。通式（2）通式（1）通式（3）通式（4）通式（5）或通式（6）因此，式（5）或（6）表示的光学活性氨基醇衍生物具有令人满意的光学纯度，其可用作药物，农药等的中间体，可以以低成本从天然α-氨基酸稳定地立体选择性地制备，作为容易获得，廉价的原料而不引起外消旋化。还提供：由式（3）表示的光学活性的5-羟基恶唑烷衍生物和由式（4）表示的氨基酮衍生物，它们是该生产的重要中间体; 以及制造这些的方法。

47. 发明申请

WO0220558A2 METHOD FOR BINDING, IN SOLUTION, A PEPTIDE AND A LIPOPHILIC VECTOR AND USES THEREOF 审中-公开
标题翻译：用于结合，解决方案，肽和脂质载体的方法及其用途
公开(公告)号：WO0220558A2
公开(公告)日：2002-03-14
申请号：PCT/FR0102787
申请日：2001-09-07
申请人： PASTEUR INSTITUT , CENTRE NAT RECH SCIENT , BONNET DOMINIQUE , BOUREL LINE , MELNYK OLEG
发明人： BONNET DOMINIQUE , BOUREL LINE , MELNYK OLEG
IPC分类号： A61K38/00 , A61K38/12 , A61K47/48 , C07C235/74 , C07D263/04 , C07D498/04 , C07K1/02 , C07K1/107 , C07K7/06 , C07K14/57
CPC分类号： C07D263/04 , A61K38/00 , A61K47/54 , C07C235/74 , C07K1/1077
摘要： The invention concerns a method for binding, in solution, at least a peptide composition and at least a lipophilic vector bearing an aldehyde function, said coupling comprising a step which consists in producing a hydrazone bond between said peptide compound and said lipophilic vector. The invention also concerns lipophilic vectors for use in said method, lipopeptides obtained by said method, uses of said lipopeptides for cell screening, and the applications of the invention, in particular for preparing targeting of an active principle of the peptide kind (for example hormone or neuropeptide) through physiological barriers such as cell membranes.
摘要翻译：本发明涉及在溶液中结合至少一种肽组合物和至少一种具有醛官能团的亲脂性载体的方法，所述偶联包括在所述肽化合物和所述亲脂性载体之间产生腙键的步骤。本发明还涉及用于所述方法的亲脂性载体，通过所述方法获得的脂肽，所述脂肽用于细胞筛选的用途，以及本发明的应用，特别是用于制备肽类活性成分（例如激素或神经肽）通过生理屏障如细胞膜。

48. 发明申请

WO01094322A1 4-BENZYL-2-HYDROXY-1,4-OXAZIN-3-ONE AND POLYMORPHIC FORMS THEREOF 审中-公开
标题翻译： 4-苄氧基-2-羟基-1,4-氧杂环辛烷-3-酮及其多晶型
公开(公告)号：WO01094322A1
公开(公告)日：2001-12-13
申请号：PCT/US2001/018038
申请日：2001-06-04
IPC分类号： C07D263/04 , C07D265/32 , C07D263/06
CPC分类号： C07D263/04 , C07D265/32
摘要： The present invention is concerned with 4-benzyl-2-hydroxy-1,4-oxazin-3-one, and novel processes for the preparation therof. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
摘要翻译：本发明涉及4-苄基-2-羟基-1,4-恶嗪-3-酮及其制备方法。该化合物可用作合成具有药理活性的化合物的中间体。

49. 发明申请

WO01045703A1 NITROSATED AND NITROSYLATED CYCLOOXYGENASE-2 INHIBITORS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：硝酸和硝基环己烷-2抑制剂，组合物和使用方法
公开(公告)号：WO01045703A1
公开(公告)日：2001-06-28
申请号：PCT/US2000/035014
申请日：2000-12-22
IPC分类号： C07D207/325 , A61K31/165 , A61K31/201 , A61K31/216 , A61K31/222 , A61K31/40 , A61K31/404 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/437 , A61K31/445 , A61K31/454 , A61K31/50 , A61K45/00 , A61P1/00 , A61P1/04 , A61P7/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/02 , A61P13/12 , A61P15/04 , A61P15/08 , A61P17/02 , A61P19/02 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P35/02 , A61P43/00 , C07C317/44 , C07C317/46 , C07C323/01 , C07C381/00 , C07D207/32 , C07D207/333 , C07D209/12 , C07D209/18 , C07D209/28 , C07D211/54 , C07D231/06 , C07D231/12 , C07D231/14 , C07D233/54 , C07D237/14 , C07D261/08 , C07D263/06 , C07D263/20 , C07D263/32 , C07D311/12 , C07D311/66 , C07D413/12 , C07D471/04 , C07D263/04
CPC分类号： C07D207/333 , C07C317/46 , C07C381/00 , C07D209/12 , C07D209/18 , C07D231/12 , C07D231/14 , C07D233/64 , C07D237/14 , C07D261/08 , C07D263/20 , C07D307/58 , C07D311/12 , C07D413/12 , C07D471/04
摘要： The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound taht donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or optionally, at least one therapeutic agent, such as, steroids, nonsteroidal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The present invention also provides novel compositions comprising at least one parent COX-2 inhibitor and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The present invention also provides kits and methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity; and for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2.
摘要翻译：本发明描述了新的亚硝化和/或亚硝基化的环氧合酶2（COX-2）抑制剂和包含至少一种亚硝化和/或亚硝基化的环氧合酶2（COX-2）抑制剂和任选的至少一种化合物供体的新组合物，转移或释放一氧化氮，刺激一氧化氮的内源性合成，提高内源性内皮衍生的松弛因子水平，或者是一氧化氮合酶的底物，和/或任选地至少一种治疗剂，例如类固醇，非甾体抗炎化合物（NSAID），5-脂氧合酶（5-LO）抑制剂，白细胞三烯B4（LTB4）受体拮抗剂，白细胞三烯A4（LTA4）水解酶抑制剂，5-HT激动剂，3-羟基-3-甲基戊二酰辅酶A（HMG-CoA），H2拮抗剂，抗肿瘤剂，抗血小板剂，减充血剂，利尿剂，镇静剂或非镇静抗组胺药，诱导型一氧化氮合酶抑制剂，阿片样物质，镇痛药，幽门螺杆菌< 抑制剂，质子泵抑制剂，异雄甾烷抑制剂及其混合物。本发明还提供了包含至少一种母体COX-2抑制剂和至少一种一氧化氮供体以及任选的至少一种治疗剂的新型组合物。本发明还提供用于治疗炎症，疼痛和发烧的试剂盒和方法; 用于治疗和/或改善COX-2抑制剂的胃肠性质; 促进伤口愈合; 用于治疗和/或预防肾毒性; 并且用于治疗和/或预防由环氧合酶-2水平升高引起的其它疾病。

50. 发明申请

WO01034594A1 DIPEPTIDYL PEPTIDASE IV INHIBITORS AND METHODS OF MAKING AND USING DIPEPTIDYL PEPTIDASE IV INHIBITORS 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE IV抑制剂及其制备和使用DIPEPTIDYL肽酶IV抑制剂的方法
公开(公告)号：WO01034594A1
公开(公告)日：2001-05-17
申请号：PCT/US2000/030836
申请日：2000-11-13
IPC分类号： C12N9/99 , A61K31/401 , A61K31/4439 , A61K38/00 , A61K38/55 , A61K45/00 , A61P9/10 , A61P13/08 , A61P25/00 , A61P25/06 , A61P25/16 , A61P35/00 , A61P43/00 , C07C229/46 , C07C237/12 , C07C255/46 , C07C327/42 , C07D207/16 , C07D233/02 , C07D241/04 , C07D257/04 , C07D263/06 , C07D277/06 , C07D279/12 , C07D307/24 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/04 , C07D417/04 , C07F9/40 , C07F9/48 , C07F9/572 , C07K5/062 , C07D401/06 , A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/421 , A61K31/426 , C07D207/12 , C07D233/14 , C07D263/04 , C07D277/04
CPC分类号： C07D257/04 , C07C229/46 , C07C237/12 , C07C255/46 , C07C327/42 , C07C2601/08 , C07D207/16 , C07D233/02 , C07D241/04 , C07D263/06 , C07D277/06 , C07D279/12 , C07D307/24 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/04 , C07D417/04 , C07F9/4006 , C07F9/4833 , C07F9/5726
摘要： The present invention provides the inhibitors of dipeptidyl peptidase IV based upon or including proline or similar moieties. The inhibitors are useful for treating various disorders, including those of the central nervous system and the prostate. Many of the inhibitors can be reversible, and can cross the blood-brain barrier. Methods of making and using the inhibitors and treatment methods also are provided.
摘要翻译：本发明提供了基于或包括脯氨酸或类似部分的二肽基肽酶IV的抑制剂。抑制剂可用于治疗各种疾病，包括中枢神经系统和前列腺疾病。许多抑制剂可以是可逆的，并且可以穿过血脑屏障。还提供了制备和使用抑制剂的方法和处理方法。

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